Difference between revisions of "Diflunisal"

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Diflunisal
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187px
Systematic (IUPAC) name
2',4'-difluoro-4-hydroxybiphenyl-3-carboxylic acid
Clinical data
Pregnancy
category
  • AU: C
  • US: C (Risk not ruled out)
Routes of
administration		 Oral
Legal status
Legal status
Pharmacokinetic data
Bioavailability 80-90%
Protein binding >99%
Metabolism Hepatic
Biological half-life 8 to 12 hours
Excretion Renal
Identifiers
CAS Number 22494-42-4
ATC code N02BA11 (WHO)
PubChem CID 3059
DrugBank APRD00922
ChemSpider 2951
Chemical data
Formula C13H8F2O3
Molar mass 250.198 g/mol[[Script error: No such module "String".]]
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'Diflunisal' is a generic NSAID (non-steroidal anti-inflammatory drug). It was developed by Merck Sharp & Dohme in 1971 after showing promise in a research project studying more potent chemical analogs of aspirin.[1] It was first sold under the brand name Dolobid, marketed by Merck & Co., but generic versions are now widely available. It is available in 250 mg and 500 mg tablets.

Mechanism

Like all NSAIDs, Diflunisal acts by inhibiting the production of prostaglandin [2], a hormone which is involved in inflammation and pain. There is also an antipyretic effect, but this is not a recommended use of the drug. Though diflunisal has an onset of 1 hour, and maximum analgesia at 2 to 3 hours, the diflunisal plasma levels will not be steady until repeated doesages are achieved. The long plasma half-life is a distinctive feature of diflunisal in comparison to similar drugs. To increase the rate at which the diflunisal plasma levels become steady, a loading dose is usually used. It is primarily used to treat symptoms of arthritis, and for acute pain following oral surgery, especially removal of wisdom teeth.

Effectiveness of diflunisal is similar to other NSAIDs, but duration of action is twelve hours or more. [3] This means fewer doses per day are required for chronic administration. In acute use, it is popular in dentistry when a single dose after oral surgery can maintain analgesia until the patient is asleep that night.

Side Effects

The inhibition of prostaglandins also has the effect of decreasing the protection given to the stomach from its own acid. Like all NSAIDS, this leads to an increased risk of stomach ulcers, and their complications, with long-term use.

Overdose

Deaths that have occurred from diflunisal usually involved mixed drugs and or extremely high dosage. The oral LD50 is 500 mg/kg. Symptoms of overdose include coma, tachycardia, stupor, and vomiting. The lowest dose without the presence of other medicines which caused death was 15 grams. Mixed with other medicines, a death at 7.5 grams has also occurred. Diflunisal usually comes in 250 or 500 mg, thus it is relatively hard to overdose by accident.


Indicated for:
  • Pain, mild-moderate
  • Osteoarthritis
  • Rheumatoid arthritis
  • Injury to tendons
  • Inflammation

Do not cut/crush/chew. Monitor blood pressure. Use lowest effective dose for shortest duration.

Side effects:

Cardiovascular:

  • Irregular heart beat (!)
  • This medication may increase risk of serious and potentially fatal cardiovascular thrombotic events, MI, and stroke (!)
  • Risk may increase with duration of use (!)
  • Increased risk for Cardiovascular disease history (!)
  • Contraindicated for Heart Bypass peri-op pain (!)

Ear, nose, and throat:

  • Ringing in the ears (!)

Eye:

  • Yellowing of eyes (!)

Gastrointestinal:

  • Increased risk of serious GI adverse events including bleeding, ulceration, and stomach or intestine perforation which can be fatal: may occur at any time during use and without warning. Elderly at greater risk for serious GI events (!)
  • Abdominal pain and cramps
  • Constipation
  • Gas & Flatulence
  • Diarrhea
  • Nausea & Vomiting
  • Dyspepsia

Central Nervous System:

  • Drowsiness
  • Dizziness
  • Headache
  • Insomnia
  • Fatigue
  • Somnolence

Psychiatric:

  • Nervousness

Skin:

  • Swelling of the feet, ankles, lower legs, and hands (!)
  • Yellowing of skin (!)
  • Rash
  • Ecchymosis

Contraindications:

  • Hypersensitivity to aspirin/NSAID-induced asthma or urticaria
  • Aspirin triad
  • Pregnancy 3rd trimester
  • CABG surgery (peri-op pain)

Cautions:

  • Cardiovascular disease
  • Cardiac risk factors
  • Hypertension
  • Congestive Heart Failure
  • Elderly or debilitated
  • Impaired liver function
  • Impaired kidney function
  • Dehydration
  • Fluid retention
  • GI bleed history/PUD
  • Asthma
  • Coagulopathy
  • Smoker
  • Corticosteriod use
  • Anticoagulant use
  • Alcohol use
  • Diuretic use
  • ACE Inhibitor use
  • Prolonged use

Precautions:

  • If symptoms labeled, (!), appear, stop usage immediately and contact your doctor.
  • Overdose is possible and deaths have occurred.
  • Do not take while on other pain medications.
  • Do not take while pregnant or breast feeding.

References

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External links

Pyrazolidine/Butylpyrazolidines
Acetic acid derivatives
and related substances
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M: MUS, DF+DRCT

anat (h/n, u, t/d, a/p, l)/phys/hist

noco(m, s, c)/cong(d)/tumr, sysi/epon, injr

proc, drug (M1A/3)

Non-steroidal anti-inflammatory drug (NSAID) products (primarily M01A and M02A, also N02BA)
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Arylalkanoic acids
2-Arylpropionic acids
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N-Arylanthranilic acids
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Items listed in bold indicate initially developed compounds of specific groups. †Withdrawn drugs. ‡Veterinary use medications.
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See also: Opioids template
Opium & alkaloids thereof
Semi-synthetic opium
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Anthranilic acid
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Atypical, Adjuvant & Potentiators,
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es:Diflunisal

it:Diflunisal pl:Diflunisal pt:Diflunisal

vi:Diflunisal
  1. ↑ Ibuprofen, the propionics and NSAIDs: Personal reflections over four decades Inflammopharmacology, Volume 7, Number 3 / September, 1999 url=http://www.springerlink.com/index/X417H50243123X78.pdf retrieved Aug 12, 2009 doi:10.1007/s10787-999-0002-3
  2. ↑ Physiol. Rev. 88: 1547-1565, 2008; doi:10.1152/physrev.00004.2008
  3. ↑ http://www2.cochrane.org/reviews/en/ab007440.html
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